methylprednisolone
Brand: Solu-Medrol, Medrol, Depo-Medrol
Prototype: prednisone
Drug Class: corticosteroid
Drug Family: corticosteroid
Subclass: synthetic glucocorticoid (intermediate-acting)
Organ Systems: endocrineimmunology
Mechanism of Action
Synthetic glucocorticoid with 5 times the anti-inflammatory potency of hydrocortisone and minimal mineralocorticoid activity. Binds GR to broadly suppress gene transcription of inflammatory cytokines, upregulate anti-inflammatory proteins, and inhibit immune cell trafficking and activation.
glucocorticoid receptor (GR)
Indications
- severe acute asthma exacerbations (IV)
- autoimmune diseases (multiple sclerosis, SLE, IBD flares)
- transplant rejection prophylaxis
- anaphylaxis (secondary to epinephrine)
- spinal cord injury (historical; no longer standard of care)
- cerebral edema reduction
Contraindications
- systemic fungal infections
- hypersensitivity to methylprednisolone
Adverse Effects
Common
- hyperglycemia
- fluid retention
- insomnia
- mood changes
Serious
- adrenal suppression
- avascular necrosis
- peptic ulcer
- myopathy
- Cushing's syndrome
- opportunistic infections
Pharmacokinetics (ADME)
| Absorption | oral, IV, IM; Solu-Medrol is water-soluble for IV use; Depo-Medrol is long-acting repository for intra-articular injection |
| Distribution | widely distributed; crosses BBB and placenta |
| Metabolism | hepatic CYP3A4 |
| Excretion | renal |
| Half-life | 2.5–3.5 hours (plasma); 12–36 hours (biologic) |
| Onset | IV: minutes; oral: 1–2 hours |
| Peak | varies |
| Duration | 12–36 hours (biologic effect) |
| Protein Binding | 77% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 inhibitors | increased methylprednisolone exposure | moderate |
| NSAIDs | additive GI ulceration | major |
| live vaccines | contraindicated during immunosuppressive doses | major |
Nursing Considerations
- For acute asthma or COPD exacerbation: IV methylprednisolone 125 mg used in emergency settings; oral prednisone sufficient for outpatient treatment.
- Administer with food to reduce GI irritation; consider GI protective agents (PPIs) for prolonged use.
- Taper dose slowly when discontinuing after prolonged use (>1–2 weeks) to prevent adrenal insufficiency; provide patient education on recognizing withdrawal symptoms.
- For pulse therapy (high-dose IV): monitor blood pressure, blood glucose, and potassium closely during infusion.
Clinical Pearls
- Solu-Medrol (methylprednisolone sodium succinate) is the IV formulation of choice for most acute indications (asthma, MS exacerbations, organ transplant rejection) due to its high water solubility and rapid onset.
- Depo-Medrol (methylprednisolone acetate) is a depot formulation used for intra-articular or intramuscular injections; it should NEVER be injected IV or intrathecally (fatal neurotoxicity).
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
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